Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract: A process for preparing compounds of the formula ##STR1## wherein X is O or S; n is one or two; m is zero or one; Y is CH.sub.2, O, or S provided that Y is O or S only when m is one; and A is ##STR2## is disclosed. Also disclosed are processes for preparing the corresponding amino intermediates.

Abstract: Metal-containing steroid mimic complexes are provided. Compositions containing a metal ion incorporated into a steroid skeleton structure and ligands useful in the preparation of such compositions are also provided. The metal ion is preferably a radionuclide, such as technetium, rhenium or gallium. Methods for using the metal complexes for diagnostic and therapeutic purposes are further provided.

Abstract: Compounds represented by the formula (I) and pharmacologically acceptable salts thereof: ##STR1## These compounds have little extrapyramidal effect and thus are effective as an anti-psychotic agent having few side effects.

Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.

Abstract: The invention relates to herbicidal sulfonylurea compounds, agriculturally suitable compositions thereof and a method for their use as general or selective preemergent or postemergent herbicides or plant growth regulants.

Abstract: Novel compounds which are 2,6-methano-2H-1-benzoxocincarboxamides having 5-HT.sub.3 -antagonist properties including unique CNS, antiemetic and gastric prokinetic activities and which are void of any significant D.sub.2 receptor binding affinity, therapeutic compositions and methods of treatment of disorders which result from 5-HT.sub.3 activity using said compounds. Processes for their preparation and the preparation of their intermediates are also disclosed.

Abstract: Azabicyclo derivatives of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is a group of formula (a), (b) or (c): ##STR2## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.10 alkyl, aralkyl or di(C.sub.1 -C.sub.4) alkylamino(C.sub.1 -C.sub.6)alkyl;R.sub.2, R.sub.3 and R.sub.4 may be the same or different and each is hydrogen, amino, halogen, C.sub.1 -C.sub.4 alkoxy or phthalimide;X is O or NH;R is C.sub.1 -C.sub.4 alkyl; andY is NR, O or S;having 5-HT.sub.3 receptor antagonist activity.

Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.

Abstract: Azabicyclo derivatives of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is a group of formula (a), (b) or (c): ##STR2## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.10 alkyl, aralkyl or di(C.sub.1 -C.sub.4) alkylamino(C.sub.1 -C.sub.6)alkyl;R.sub.2, R.sub.3 and R.sub.4 may be the same or different and each is hydrogen, amino, halogen, C.sub.1 -C.sub.4 alkoxy or phthalimide; X is O or NH;R is C.sub.1 -C.sub.4 alkyl; andY is NR, O or S;having 5-HT.sub.3 receptor antagonist activity.

Abstract: The invention relates to new anilino iminoazoles and iminoazines of general formula I ##STR1## in which A, B, D, E, W, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Rr.sup.5 have the meanings given in the description, processes for their preparation and their use as herbicides.

Abstract: Novel 3-aryl-pyrrolidine 2,4-dione derivatives of the formula ##STR1## having pesticidal activity.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen;either R.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylithio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O)n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.

Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene- , furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide. 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.

Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen; either R.sub.1 is C.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O) n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.

Abstract: The compound having the formula: ##STR1## wherein R.sup.6 is a hydrogen atom or an alkanoyl group, or a salt thereof and a process thereof.

Abstract: This invention relates to herbicidally active sulfonamide compounds having an ortho cyclic saturated or partially saturated group which includes a carbonyl or sulfonyl radical.

Abstract: Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which X is --O--, --S--, --SO--, --SO.sub.2 --, --CR.sub.3 R.sub.4 --where R.sub.3 and R.sub.4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R.sub.3 and R.sub.4 form a cycloalkyl group of 3 to 5 carbon atoms; Y is alkylene of 1 to 3 carbon atoms or alkenylene of 2 to 3 carbon atoms; n is one of the integers 0 to 1; m is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; or a pharmaceutically acceptable salt thereof.

Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,3-dihydro-6-methyl-3-oxof uro[3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.

Abstract: This invention relates to novel isoxazolo-pyrido-benzoxazine and isothiazolo-pyrido-benzoxazine derivatives having antibacterial properties.

Abstract: The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, andeither A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine optionally substituted by OH, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 2,3-dihydropyrrolo[2,1-b]thiazole, 1H,3H-pyrrolo[1,2-c]oxazole, 1,2-dihydro-4H-pyrrolo]1,2-c]-1,3-oxazine or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, n=0 or 1, Het=3-pyridyl or 5-thiazolyl, and(1) either R=H, halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio and Y=alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, or Y=--NR.sub.1 R.sub.2 with:either R.sub.1 =H and R.sub.2 =unsubstituted alkyl, cycloalkyl (C.sub.3 -C.sub.6), alkenyl (C.sub.2 -C.sub.4), alkynyl (C.sub.3 -C.sub.

Abstract: Benzylsulfonylureas and arylsulfamoylureas are useful as pre-emergent and post-emergent herbicides and as plant growth regulants.

Abstract: Substituted 2-amino-4(1H)pyridones are provided which are renal vasodilators and bronchodilators.

Abstract: Antithrombotics of the formula ##STR1## in which A=S, SO or SO.sub.2, R.sub.3 =H, alkyl or substituted or unsubstituted phenyl, X=O, S, NH or variously substituted nitrogen, p is 0 or 1 and y=H, NH.sub.2, or various substituted amines.

Abstract: The invention provides new derivatives of the formula: ##STR1## in which either (a) Y=COOH or a radical of the formula (II), in which R.sub.2 =alkyl or benzyl, A=a sulphur atom, m=1, n=0, R=pyridin-3-yl and R.sub.1 =H, or (b) Y=CN, COOH or a radical of the formula ##STR2## defined as above, A=S, O or CH.sub.2, m=1 or 2 and n=0, 1 or 2, (m+n) being 1, 2 or 3, R=H, alkyl or phenyl (optionally substituted by halogen, alkyl, alkoxy or CF.sub.3) and R.sub.1 =a radical of the formula ##STR3## in which p=0 or 1, the alkyl radicals and alkyl portions being straight-chain or branched-chain and containing 1 to 4 carbon atoms each. Processes for the production of these compounds are described. They are useful as intermediates for the preparation of new medicaments.

Abstract: Tricyclic antidepressant drug (e.g., imipramine, desipramine, amitriptyline, or nortriptyline) immunogens, antibodies prepared therefrom, labeled conjugates, synthetic intermediates, and the use of such antibodies and labeled conjugates in immunoassays for determining such drug. The immunogens comprise the drug coupled at its 2'-position to an immunogenic carrier material. Similarly, the labeled conjugates and synthetic intermediates are 2'-derivatives of the drug or a precursor thereof. The antibodies and labeled reagents are particularly useful in certain homogeneous nonradioisotopic immunoassays for measuring tricyclic antidepressant drugs in biological fluids such as serum.

Abstract: Novel syn isomers of optically active isomers and racemates of 7-[2-(2-amino-4-thiazolyl)-2-oxyimino-acetamido]-bicyclooctene-carboxylic acid derivatives of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, methyl, halomethyl, hydroxymethyl and acyloxymethyl, X is selected from the group consisting of oxygen and optionally oxidized sulfur, A is selected from the group consisting of hydrogen, an alkali metal, --NH.sub.4, alkaline earth metal equivalent, a non-toxic, pharmaceutically acceptable organic amine and an easily cleavable ester group and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic activity and their preparation.

Abstract: A process is described whereby a synthetically produced 4-styryl-cis-3,4-azetidinone is converted to an isocephalosporin or its 2-oxa analog. The process is based upon the condensation of enamine and imine synthons. Novel intermediate azetidinones are also disclosed. Control of the stereochemical course of the process allows economical, high yield preparation of the racemic form of the product or when a single enantiomer of the imine synthon derived from the .beta.-hydroxy-.alpha.-amino acid starting material is used, both enantiomers of the product may be prepared and separated without optical resolution.

Abstract: Compounds having the formula: ##STR1## wherein X.sub.1, X.sub.2, R, R.sub.1, R.sub.2 and R.sub.3 are as set forth hereinafter, their preparation and uses as ganglionic blocking agents are disclosed.

Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is oxygen or sulphur;R.sub.1 is a C.sub.1-6 alkoxy or C.sub.1-6 alkylthio group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.2 and R.sub.3 above;R.sub.4 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.5 where s is 0 to 2 and R.sub.5 is a C.sub.3-8 cycloalkyl group, or a group --(CH.sub.2).sub.t R.sub.6 where t is 1 or 2 and R.sub.6 is a phenyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.

Abstract: Aryl-1-mercaptoalkanoylproline and homoproline derivatives and their cyclized thiazadione heterocyclic analogues reduce blood pressure in animals by ACE inhibition.

Abstract: 6,7-Dihydro-8H-pyrrolo[2,1-c][1,4]thiazine-1(8aH),4(3H)-dione is useful as an inhibitor of Angiotensin I converting enzyme.

Abstract: Triazolone herbicides of the formula: ##STR1## where V is hydrogen, fluorine, chlorine, bromine, methyl or OR where R is alkyl of 1-4 carbon atoms;X is hydrogen, fluorine, chlorine, bromine, cyano, methyl, methoxy, or nitro;Y is hydrogen, fluorine, chlorine, bromine, or methyl;N, m is 0, 1, 2, 3 or 4;Q is oxygen or sulfur;Z is oxygen, S(O).sub.p or NR';p is 0, 1 or 2 andR' is alkyl of 1-3 carbon atomsWith the provisos that(1) n + m = 2, 3, or 4; and(2) if n + m = 2 or 4 then Y, X .noteq. Hand when Z is S(O).sub.p, n is 1, 2, 3 or 4.

Abstract: Novel bicyclic .beta.-lactams and intermediates useful in their preparation are disclosed. In particular, 7.beta.-acyl-amino- and 7.beta.-amino-8-oxo-4-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acids are prepared. The acylated compounds are antibacterial agents.

Abstract: The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.

Abstract: Synthetic ester lubricant blends are described which contain 1-90 weight percent of an N-substituted polyoxyalkylene phenothiazine. The polyoxyalkylene group can be derived from ethylene, propylene, butylene or styrene oxides. The blends have superior oxidative and thermal stability and at the same time have good viscosity characteristics and pour points over a wide range of temperatures.